Nilotinib was first disclosed in U.S. Pat. No. 7,169,791. It is chemically described as 4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-benzamide and is an inhibitor of the protein tyrosine kinase (TK) activity of BCR-ABL.
U.S. Pat. No. 8,293,756 discloses pharmaceutical compositions of nilotinib prepared by wet granulation.
Nilotinib is characterized as a Class IV compound according to the Biopharmaceutical Classification System (BCS), which means that it has low/moderate aqueous solubility and low permeability. The solubility of nilotinib at 25° C. in aqueous solutions decreases strongly with increasing pH and it is practically insoluble at pH 4.5 and higher. This decrease in the solubility of nilotinib in environments with a pH of more than 1 leads to a decrease in the absorption of nilotinib. The poor water-solubility of nilotinib and its salts mean that they are difficult to formulate as oral delivery dosage forms with good bioavailability. Hence, there is a need to develop a pharmaceutical solid oral dosage form of nilotinib which has better solubility and bioavailability. In the present invention, the inventors have developed such a pharmaceutical oral solid dosage form of nilotinib.